近日，美国食品和药物管理局（FDA）提前2个月批准Eucrisa（crisaborole，2%）软膏，作为一种局部外用药物，用于2岁及以上儿童和成人患者轻度至中度特应性皮炎（湿疹，eczema）的治疗。
特应性皮炎是一种常见的复发性慢性炎性皮肤疾病，患者通常表现为以炎症和瘙痒为特点的慢性皮疹，好发于皮肤褶皱处，症状通常会持续14天以上。据估计，在美国大约有2500万人受特应性皮炎（湿疹）困扰，其中婴儿和儿童占8%~18%。目前，特应性皮炎缺少有效的治疗药物。
FDA的药品评价和研究中心(CDER)中药品评价III办公室副主任Amy Egan说："今天的批准为处理轻度至中度异位性皮炎患者提供另一种治疗选择。"
批准日期：2016年12月14日,公司：Pfizer，Inc.
EUCRISA™(crisaborole)软膏，2%，为局部使用
美国初次批准：2016
作用机制
Crisaborole是一个磷酸二酯酶4(PDE-4)抑制剂。PDE-4抑制作用导致增加细胞内环化腺苷一磷酸(cAMP)水平。Crisaborole 发挥其对异位性皮炎的治疗作用的特异性机制尚未很好确定。
适应证和用途
EUCRISA是一种磷酸二酯酶4抑制剂适用为在2岁和以上患者轻度至中度异位性皮炎[atopic dermatitis]的局部治疗。
剂量和给药方法
● 对受影响区域应用一薄层每天2次。
● 仅为局部使用。
● 不为眼科，口服或阴道内使用。
剂型和规格
软膏，2%。
禁忌证
已知对crisaborole或制剂的任何组分超敏性。
警告和注意事项
超敏反应：如发生超敏性体征和症状，立即终止EUCRISA和开始适当治疗。
不良反应
最常见不良反应发生在≥1%受试者是应用部位疼痛。
供应/贮存和处置
供应
EUCRISA是一个白色至米白色软膏含2% crisaborole和在60g和100g层压管中供应。
60g管：NDC 55724-211-21
100g管：NDC 55724-211-11

Pfizer Receives FDA Approval for EUCRISA™ (crisaborole), a Novel Non-Steroidal Topical Ointment for Mild to Moderate Atopic Dermatitis (Eczema)
U.S. Food and Drug Administration (FDA) approved EUCRISATM (crisaborole) ointment 2%, a novel non-steroidal topical phosphodieterase-4 (PDE-4) inhibitor for the treatment of mild to moderate atopic dermatitis (AD) in patients two years of age and older.1 AD, often called eczema, is a chronic condition impacting nearly 18 million children and adults in the United States.2 Approximately 90 percent of people living with AD have the mild to moderate form of the condition.
“The approval of EUCRISA is great news for the children and adults suffering from mild to moderate eczema, a community that has not had a new prescription treatment for more than 10 years,” said Albert Bourla, Group President, Pfizer Innovative Health. “This is also an important milestone for Pfizer as we continue to build on our heritage in Inflammation and Immunology by offering innovative treatment options to patients who need them.”
EUCRISA is the first and only non-steroidal topical monotherapy that inhibits the PDE-4 enzyme in the skin. Overactive PDE-4 has been shown to contribute to the signs and symptoms of AD.4 The specific mechanism of action of crisaborole in AD is not well defined.
“I’m delighted to have a new option for my patients with mild to moderate atopic dermatitis,” said Amy Paller, M.D., Walter J. Hamlin Professor and Chair of Dermatology, Professor of Pediatrics, Northwestern University Feinberg School of Medicine, a clinical trial investigator. “The results seen in these pivotal Phase 3 studies show the efficacy and safety of EUCRISA as a steroid-free treatment option for people as young as two living with mild to moderate atopic dermatitis.”
SELECTED IMPORTANT SAFETY INFORMATION
CONTRAINDICATION: EUCRISA is contraindicated in patients with known hypersensitivity to crisaborole or any component of the formulation.
EUCRISA TRIAL RESULTS
The approval of EUCRISA is based on a clinical development program including the results of two large, identical, multicenter, randomized, double-blind, parallel-group, vehicle- controlled (non-medicated ointment) trials (Trials 1 and 2) that treated 1,522 patients with mild to moderate AD between the ages of two and 79.1 At baseline, 38.5% of the subjects had an Investigator’s Static Global Assessment (ISGA) score of 2 (mild), and 61.5% had an ISGA score of 3 (moderate). The ISGA score includes erythema (redness), induration (hardening)/papulation (formation of papules), and oozing/crusting on a severity scale of 0 to.
In both trials, subjects were randomized 2:1 to receive EUCRISA or vehicle (non-medicated ointment) applied to skin with signs and symptoms of AD twice daily for 28 days.1 The primary efficacy endpoint was success in ISGA at day 29, defined as the proportion of patients achieving an ISGA score of 0 (clear) or 1(almost clear) with at least a 2-grade improvement from baseline. These data showed EUCRISA to be an effective treatment that achieved statistically significant results versus vehicle for the primary efficacy endpoint in adults and children two years of age and older [32.8% versus 25.4% (P=0.038) for Trial 1 and 31.4% versus 18.0% (P<0.001) for Trial 2].1,3 Efficacy results were seen in some patients as early as day eight (first post-baseline assessment), with 13.4% of EUCRISA patients achieving success in ISGA versus 4.5% with vehicle in Trial 1 and 15.9% EUCRISA versus 6.3% vehicle in Trial
In these studies, the adverse reaction reported by more than 1% of EUCRISA patients was pain at the application site, such as stinging or burning [4% (N=45)] versus vehicle [1% (N=6)]. The rate of study discontinuation due to adverse reactions was the same in the EUCRISA group versus vehicle (1.2%).
“After many years without new therapies, this is an exciting day for those living with mild to moderate eczema and their caregivers,” said Julie Block, President and Chief Executive Officer of the National Eczema Association.
INDICATION & IMPORTANT SAFETY INFORMATION
INDICATION
EUCRISA is indicated for topical treatment of mild to moderate atopic dermatitis in patients 2 years of age and older.
CONTRAINDICATIONS
EUCRISA is contraindicated in patients with known hypersensitivity to crisaborole or any component of the formulation.
WARNINGS AND PRECAUTIONS
Hypersensitivity reactions, including contact urticaria, have occurred in patients treated with EUCRISA and should be suspected in the event of severe pruritus, swelling and erythema at the application site or at a distant site. Discontinue EUCRISA immediately and initiate appropriate therapy if signs and symptoms of hypersensitivity occur.
ADVERSE REACTIONS
The most common adverse reaction occurring in ≥ 1% in subjects in clinical trials was application site pain, such as burning or stinging.
The full results for these trials were published in July 2016, in the Journal of the American Academy of Dermatology.
For Full Prescribing Information please visit www.pfizer.com.
About Atopic Dermatitis
Atopic dermatitis is a chronic condition characterized by inflammation of the skin.2 Lesions of atopic dermatitis are characterized by erythema (redness), induration (hardening)/papulation (formation of papules), and oozing/crusting.
About EUCRISATM (crisaborole) ointment 2%
EUCRISA is a prescription ointment used on the skin (topical) to treat mild to moderate atopic dermatitis (commonly referred to as eczema) in adults and children two years of age and older.